تفاعل #67143

معادلة التفاعل

N-(2-Chloro-5-{4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-[(4-methylphenyl)sulfonyl]-1H-indazol-6-yl}-3-pyridinyl)methanesulfonamide

(2R,6S)-2,6-dimethylmorpholine

→

title compound

المردود 27.6%

N-{2-Chloro-5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3,4-oxadiazol-2-yl)-1H-indazol-6-yl]-3-pyridinyl}methanesulfonamide

المردود 27.6%

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةThe reaction was heated in the microwave for a further 20 mins
2. 2
   أخرىThe (2R,6S)-2,6-dimethylmorpholine was removed
3. 3
   أخرىThe solvent was removed
4. 4
   أخرىthe residue purified by Mass Directed Automated Preparative HPLC (Method B)
5. 5
   أخرىThe desired product was not collected so the waste
6. 6
   تركيزwas concentrated in vacuo
7. 7
   أخرىthe residue purified by Mass Directed Automated Preparative HPLC (Method B)

الإجراء التجريبي

N-(2-Chloro-5-{4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-[(4-methylphenyl)sulfonyl]-1H-indazol-6-yl}-3-pyridinyl)methanesulfonamide (50 mg, 0.084 mmol) and (2R,6S)-2,6-dimethylmorpholine (0.5 ml, 0.084 mmol) were placed a vial and heated in a microwave at 90° C. for 15 mins. The reaction was heated in the microwave for a further 20 mins. The (2R,6S)-2,6-dimethylmorpholine was removed and the residue placed into isopropanol (3 ml) and 2M sodium hydroxide (1 ml) and the mixture stirred at room temperature for 3 h. The solvent was removed and the residue purified by Mass Directed Automated Preparative HPLC (Method B). The desired product was not collected so the waste was concentrated in vacuo and the residue purified by Mass Directed Automated Preparative HPLC (Method B) to give the title compound as white solid (12 mg).

المصدر